1. Metabolic Enzyme/Protease
  2. Dopamine β-hydroxylase
  3. Nepicastat

Nepicastat  (Synonyms: 内匹司他; SYN117; RS-25560-197)

目录号: HY-13289
产品使用指南

Nepicastat (SYN117) 是一种选择性的,有效的,具有口服活性的多巴胺 β 羟化酶 (dopamine-beta-hydroxylase) 抑制剂。Nepicastat (SYN117) 对牛 (IC50=8.5 nM) 和人(IC50=9 nM) 多巴胺 β 羟化酶产生浓度依赖性抑制作用。Nepicastat (SYN117) 可越过血脑屏障。

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Nepicastat Chemical Structure

Nepicastat Chemical Structure

CAS No. : 173997-05-2

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规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

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Nepicastat 的其他形式现货产品:

Other Forms of Nepicastat:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB)[1][2][3].

IC50 & Target

IC50: 8.5 nM (bovine dopamine-beta-hydroxylase), 9 nM (human dopamine-beta-hydroxylase)[2]

体内研究
(In Vivo)

Nepicastat (3-100 mg/kg; p.o.; three consecutive times, 12 hours apart times) produces dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 15-16 weeks male spontaneously hypertensive rats (SHRs)[3]
Dosage: Oral administration; three consecutive times, 12 hours apart
Administration: 3, 10, 30, 100 mg/kg
Result: Produced dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle and cerebral cortex.
Clinical Trial
分子量

295.35

Formula

C14H15F2N3S

CAS 号
中文名称

内匹司他

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 48 mg/mL (162.52 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3858 mL 16.9290 mL 33.8580 mL
5 mM 0.6772 mL 3.3858 mL 6.7716 mL
查看完整储备液配制表
  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3858 mL 16.9290 mL 33.8580 mL 84.6451 mL
5 mM 0.6772 mL 3.3858 mL 6.7716 mL 16.9290 mL
10 mM 0.3386 mL 1.6929 mL 3.3858 mL 8.4645 mL
15 mM 0.2257 mL 1.1286 mL 2.2572 mL 5.6430 mL
20 mM 0.1693 mL 0.8465 mL 1.6929 mL 4.2323 mL
25 mM 0.1354 mL 0.6772 mL 1.3543 mL 3.3858 mL
30 mM 0.1129 mL 0.5643 mL 1.1286 mL 2.8215 mL
40 mM 0.0846 mL 0.4232 mL 0.8465 mL 2.1161 mL
50 mM 0.0677 mL 0.3386 mL 0.6772 mL 1.6929 mL
60 mM 0.0564 mL 0.2822 mL 0.5643 mL 1.4108 mL
80 mM 0.0423 mL 0.2116 mL 0.4232 mL 1.0581 mL
100 mM 0.0339 mL 0.1693 mL 0.3386 mL 0.8465 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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目录号:
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